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Home Page > Alphabetical Index > TEMECHINE

TEMECHINE Prod. No L9044 - CAS # 30015-57-7
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Product Name TEMECHINE
Product Code L9044
TEMECHINE

C11H21N .HBr
Molecular Formula C11H21N .HBr
Description

a neuronal nicotinic AChR antagonist. Potent ganglioblocker. Hypotensive. Good penetration of biological membranes. Rigid bicyclic analog of Pempidine. Non-quaternary analog of Quirestine.

Quinicludine derivative‚ C11H21N .HBr ‚ synthetic.
 
Biological Activity

For comparative information see the attached 2 tables.

Cell permeant central nicotinic acetylcholine receptor blocker without action on skeleton muscle innervation. Quinuclidine analog of Pempidine‚ non-quaternary analog of Quirestine. Hypotensive‚ selectively blocks autonomic ganglia‚ the adrenal medulla‚ carotid glomerules.



Three-fold more active than Pempidine‚ wide therapeutic range [1]. Slows down neuronal pre- and post ganglionar transmission: dilates peripheral vessels and bronchi‚ arterial pressure and pressor reaction drop. Suppresses gland secretion. Sedative.



Good penetration of biological membranes.



Blocks superior cervical sympathetic ganglion (electrical stimulation of cats nictiating membrane): ED50 = 17 µg/kg ‚ Pempidine 54 µg/kg.



Blocks autonomic ganglion ( vagus electrical stimulation): depressor reaction suppression - 50 µg /kg 40%‚ 500 µg/kg 100%. After 100% nicotinic blockade with 500 µg /kg‚ cardiac system still reacts to muscarinic action of ACh (i.v.).
 
Chemical and Physical Properties
 
CAS No. 30015-57-7 Molecular Weight 248.20 Da.
RTECS Physical Form colorless crystal powder.
Merck Index No (13th Ed.) Melting point 269-273 °C.
PubChem SID Solubility water‚ ethanol (1 g in 10 ml).
Purity min. 99.5%.

TLC (Silufol UV-254‚ MeOH:NH3(25%) Rf 0.1‚ development with Dragendorff¨ reagent); NMR (D2O).		 Optical Activity
Toxicity (LD50) mice (orally): 345 mg/kg.
Chemical Names 2‚2‚6‚6-tetramethylquinicludine hydrobromide.
Storage & Reconstitution Recommendations store at room temperature. Solution for use: dissolve in water: 10-3M (2 mg in 8.06 ml)‚ stable for 1-2 days at 20°C.
Safety Recommendations do not swallow or inhale; avoid eye and skin contact.
 
Bibliographic References
  1. Mashkovsky M.D. et al., "Further developments in research on the chemistry and pharmacology of synthetic quinuclidine derivatives." Progr. Drug. Res., (1983). 27:9-61
  2. Sharapov I.V., Farm, Toksikol. (1972). (Russian). (6):687-690
  3. Nikitskaya E.S. et al., Khim. Farm. Zh. (1970) (Russian) (10):58-61
  4. Shubina L.A., Sovetskaya Med. (1968) (Russian). (10):87-92
  5. Nogaller A.M. et al., Klinitcheskaya Med. (1975) (Russian). (10):52-56
 
Prices
Code
Quantity
US $
€uro
L9044
1 x 2 mg
81.20
58.00
5 x 2 mg
324.80
232.00
 
External Links PubMed Biomedical Citations From PubMed Toxicology Citations From PubMed PubChem SID

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